High concentration olopatadine ophthalmic composition

Abstract

The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis.

We claim: 
     
       1. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
 at least 0.67 w/v % olopatadine dissolved in the solution; 
 PEG having a molecular weight of 300 to 500; 
 polyvinylpyrrolidone; 
 hydroxypropyl-γ-cyclodextrin; 
 benzalkonium chloride; and 
 water. 
 
     
     
       2. A solution as in  claim 1  further comprising borate. 
     
     
       3. A solution as in  claim 2  further comprising a polyol. 
     
     
       4. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
 at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution; 
 2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500; 
 2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone; 
 at least 0.5 w/v % but no greater than 2.0 w/v % cyclodextrin derivative selected from the group consisting of SAE-β-cyclodextrin, HP-γ-cyclodextrin, HP-β-cyclodextrin and combinations thereof; and 
 water. 
 
     
     
       5. A solution as in  claim 4  further comprising borate at a concentration of at least 0.18 w/v % but less than 0.5 w/v %. 
     
     
       6. A solution as in  claim 5  further comprising a polyol. 
     
     
       7. A solution as in  claim 6  wherein the polyol is propylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %. 
     
     
       8. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
 at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution; 
 2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500; 
 2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone; 
 at least 0.5 w/v % but no greater than 2.0 w/v % hydroxypropyl-γ-cyclodextrin; and 
 water. 
 
     
     
       9. A solution as in  claim 8  further comprising borate at a concentration of at least 0.18 w/v % but less than 0.5 w/v %. 
     
     
       10. A solution as in  claim 9  further comprising a polyol. 
     
     
       11. A solution as in  claim 10  wherein the polyol is propylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %. 
     
     
       12. A method of treating at least one ocular allergy symptom in humans, the method comprising:
 topically applying to an eye of a human an amount of the solution of  claim 4  sufficient to treat the at least one ocular allergy symptom. 
 
     
     
       13. A method as in  claim 12  wherein the step of topically applying the solution includes dispensing at least one drop of the solution to the eye. 
     
     
       14. A method as in  claim 13  wherein the at least one ocular allergy symptom includes ocular itching. 
     
     
       15. A solution as in  claim 1  further comprising hydroxypropylmethyl cellulose. 
     
     
       16. A solution as in  claim 4  further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose. 
     
     
       17. A solution as in  claim 8  further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose. 
     
     
       18. A solution as in  claim 3  wherein the polyol is mannitol. 
     
     
       19. A solution as in  claim 6  wherein the polyol is mannitol solution at a concentration that is at least 0.05 w/v % but no greater than 0.5 w/v %. 
     
     
       20. A solution as in  claim 10  wherein the polyol is mannitol at a concentration that is at least 0.05 w/v % but no greater than 0.5 w/v %. 
     
     
       21. An aqueous ophthalmic solution for treatment of ocular allergic conjunctivitis, the solution comprising:
 at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in the solution; 
 2.0 w/v % to 6.0 w/v % PEG having a molecular weight of 300 to 500; 
 2.0 w/v % to 6.0 w/v % polyvinylpyrrolidone; 
 at least 0.5 w/v % but no greater than 2.0 w/v % hydroxypropyl-γ-cyclodextrin; 
 greater than 0.003 w/v % but less than 0.03 w/v % benzalkonium chloride; and 
 water; 
 wherein the pH of the solution is 6.0 to 7.8 and the osmolality of the solution is 200 to 400 mOsm/kg. 
 
     
     
       22. A solution as in  claim 21  further comprising at least 0.15 w/v % but no greater than 1.0 w/v % hydroxypropylmethyl cellulose. 
     
     
       23. A solution as in  claim 22  wherein:
 i) the concentration of PEG is at least 3.0 w/v % but no greater than 5.0 w/v %; 
 ii) the concentration of polyvinylpyrrolidone is at least 3.0 w/v % but no greater than 5.0 w/v %; and 
 iii) the concentration of hydroxypropyl methylcellulose is at least 0.3 w/v % but no greater than 0.5 w/v %. 
 
     
     
       24. A solution as in  claim 23  further comprising:
 at least 0.18 w/v % but less than 0.4 w/v % boric acid; and 
 at least 0.05 w/v % but no greater than 0.5 w/v % mannitol. 
 
     
     
       25. A method of treating ocular allergy symptoms in humans, the method comprising:
 topically applying to an eye of a human an amount of the solution of  claim 23  sufficient to treat ocular allergy symptoms. 
 
     
     
       26. A method as in  claim 25  wherein the step of topically applying the solution includes dispensing at least one drop of the solution to the eye. 
     
     
       27. A method as in  claim 26  wherein the ocular allergy symptoms include ocular itching.